Abstract
Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) are two enzymes sensitive to various chemical compounds having ability to bind to crucial parts of these enzymes. Boldine is a natural alkaloid and it was mentioned in some older works that it can inhibit some kinds of AChE. We reinvestigated this effect on AChE and also on BChE using acetyl (butyryl) thiocholine and Ellman's reagents as standard substances for spectrophotometric assay. We found out IC50 of AChE equal to 372 μmol/l and a similar level to BChE, 321 μmol/l. We conclude our experiment by a finding that boldine is cholinesterase inhibitor; however we report significantly weaker inhibition than that suggested in literature. Likewise, we tried to investigate the mechanism of inhibition and completed it with in silico study. Potential toxic effect on cholinesterases in real conditions is also discussed.
Highlights
Cholinesterases are enzymes splitting esters of choline
In chemical terminology (S)-2,9-dihydroxy-1,10dimethoxy-aporphine (Figure 1), is a natural alkaloid with reported antioxidant activity. It was isolated from dozens of plant species from Monimiaceae and Magnoliaceae [6, 7] and recently it was reported to inhibit AChE with IC50 equal to 8.5 μmol/l [8]; it could be potential cholinesterase inhibitor
We hypothesize that boldine would serve as a structure for pharmacology research and, boldine would act as a multitarget toxin
Summary
We distinguish two enzymes belonging to the group of cholinesterases, AChE which is presented in nervous system and terminates neurotransmission and BChE occurring in serum but the particular function of the enzyme remains undiscovered [1, 2]. In chemical terminology (S)-2,9-dihydroxy-1,10dimethoxy-aporphine (Figure 1), is a natural alkaloid with reported antioxidant activity. It was isolated from dozens of plant species from Monimiaceae and Magnoliaceae [6, 7] and recently it was reported to inhibit AChE with IC50 equal to 8.5 μmol/l [8]; it could be potential cholinesterase inhibitor. We decided to investigate interaction between boldine and AChE in higher details than currently available
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